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Updated: Dec 12, 2025

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Synthesis and biological evaluation of substituted pyrrolidines and pyrroles as potential anticancer agents
Jiali Ji1, Farrukh Sajjad1, Qun You1
1Shanghai Engineering Research Centre of Molecular Therapeutics and New Drug Development, School of Chemistry and Molecular Engineering, East China Normal University, Shanghai, China.
Abstract:
A series of polysubstituted pyrrolidines obtained via ruthenium-catalyzed cascade cyclization of diazo pyruvates and anilines as well as their corresponding pyrrole analogs obtained via dehydration were evaluated for their antiproliferation activities. Pyrrolidines 3h and 3k showed good proliferation inhibitory effects toward 10 cancer cell lines with IC50 values ranging from 2.9 to 16 μM. Furthermore, pyrrolidine 3k induced cell cycle arrest at the G0/G1 phase and time- and dose-dependent cellular apoptosis in both HCT116 and HL60 cells, suggesting that this type of pyrrolidine structure might be a good candidate for future anticancer therapies.
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